BR112023000990A2 - FORMULATIONS OF DISSUPTITUTED C21-N-PYRAZOLYL 19-NOR C3,3- STEROID AND METHODS OF USE THEREOF - Google Patents

FORMULATIONS OF DISSUPTITUTED C21-N-PYRAZOLYL 19-NOR C3,3- STEROID AND METHODS OF USE THEREOF

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Publication number
BR112023000990A2
BR112023000990A2 BR112023000990A BR112023000990A BR112023000990A2 BR 112023000990 A2 BR112023000990 A2 BR 112023000990A2 BR 112023000990 A BR112023000990 A BR 112023000990A BR 112023000990 A BR112023000990 A BR 112023000990A BR 112023000990 A2 BR112023000990 A2 BR 112023000990A2
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BR
Brazil
Prior art keywords
pyrazolyl
steroid
methods
formulations
dissuptituted
Prior art date
Application number
BR112023000990A
Other languages
Portuguese (pt)
Inventor
Steven Watson Paul
Berner Bret
Narayan Padma
Chen Xiaoxia
Anthony Stutzman Todd
Meng Jianing
Wilkerson Carolyn
Ramnik Jain Raj
Original Assignee
Sage Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of BR112023000990A2 publication Critical patent/BR112023000990A2/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1611—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Anesthesiology (AREA)

Abstract

FORMULAÇÕES DE ESTEROIDE C21-N-PIRAZOLIL 19-NOR C3,3-DISSUBSTITUÍDO E MÉTODOS DE USO DAS MESMAS. Esta invenção se refere a um esteroide C21-pirazolil 19-nor C3,3-dissubstituído de fórmula (I) e composições farmacêuticas do mesmo. Também são divulgados neste documento métodos para fazer as composições farmacêuticas do esteroide C21-pirazolil 19- nor C3,3-dissubstituído de fórmula (I) e métodos para usar o esteroide C21-pirazolil 19-nor C3,3-dissubstituído de fórmula (I) ou formas sólidas cristalinas, sais farmaceuticamente aceitáveis e composições farmaceuticamente aceitáveis do mesmo.C21-N-PYRAZOLYL 19-NOR C3,3-DISSubstituted STEROID FORMULATIONS AND METHODS OF USE THEREOF. This invention relates to a C21-pyrazolyl 19-nor C3,3-disubstituted steroid of formula (I) and pharmaceutical compositions thereof. Also disclosed herein are methods for making pharmaceutical compositions of the C21-pyrazolyl 19-nor C3,3-disubstituted steroid of formula (I) and methods for using the C21-pyrazolyl 19-nor C3,3-disubstituted steroid of formula (I ) or crystalline solid forms, pharmaceutically acceptable salts and pharmaceutically acceptable compositions thereof.

BR112023000990A 2020-07-20 2021-07-20 FORMULATIONS OF DISSUPTITUTED C21-N-PYRAZOLYL 19-NOR C3,3- STEROID AND METHODS OF USE THEREOF BR112023000990A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063054070P 2020-07-20 2020-07-20
PCT/US2021/042394 WO2022020363A1 (en) 2020-07-20 2021-07-20 Formulations of 19-nor c3,3- disubstituted c21-n-pyrazolyl steroid and methods of use thereof

Publications (1)

Publication Number Publication Date
BR112023000990A2 true BR112023000990A2 (en) 2023-03-28

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Country Status (17)

Country Link
US (2) US20230285417A1 (en)
EP (1) EP4181884A1 (en)
JP (1) JP2023537240A (en)
KR (1) KR20230041049A (en)
CN (1) CN116367827A (en)
AR (1) AR123018A1 (en)
AU (1) AU2021312240A1 (en)
BR (1) BR112023000990A2 (en)
CA (1) CA3187178A1 (en)
CL (1) CL2023000176A1 (en)
CO (1) CO2023001579A2 (en)
EC (1) ECSP23012042A (en)
IL (1) IL299829A (en)
MX (1) MX2023000835A (en)
PE (1) PE20231301A1 (en)
TW (1) TW202220667A (en)
WO (1) WO2022020363A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112472814A (en) 2012-01-23 2021-03-12 萨奇治疗股份有限公司 Neuroactive steroid formulations and methods of treating central nervous system disorders
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
JP2019524853A (en) 2016-08-23 2019-09-05 セージ セラピューティクス， インコーポレイテッド Crystalline 19-nor C3,3-disubstituted C21-N-pyrazolyl steroid
KR20200096596A (en) 2017-12-08 2020-08-12 세이지 테라퓨틱스, 인크. Deuterated 21-[4-cyano-pyrazole-1-yl]-19-nor-pregan-3 for the treatment of CNS disorders. Alpha-ol-20-one derivative
AU2022238365A1 (en) 2021-03-17 2023-09-21 Sage Therapeutics, Inc. A 19-nor c3,3-disubstituted c21-n-pyrazolyl steroid for the treatment of major depressive disorder
CA3218072A1 (en) 2021-04-29 2022-11-03 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21 -n-pyrazolyl steroid for use in treating major depressive disorder and postpartum depression
IL307980A (en) 2021-04-29 2023-12-01 Sage Therapeutics Inc Neuroactive steroid for use in treating major depressive disorder and postpartum depression in a lactating female
WO2023158668A1 (en) 2022-02-16 2023-08-24 Sage Therapeutics, Inc. Neuroactive steroids for treatment of cns-related disorders
WO2023163879A1 (en) 2022-02-28 2023-08-31 Sage Therapeutics, Inc. Neuroactive steroids for treatment of gastrointestinal diseases or conditions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014169831A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof
SI2986623T1 (en) * 2013-04-17 2019-03-29 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-n-pyrazolyl steroids and methods of use thereof
JP2019524853A (en) 2016-08-23 2019-09-05 セージ セラピューティクス， インコーポレイテッド Crystalline 19-nor C3,3-disubstituted C21-N-pyrazolyl steroid
IL303250A (en) * 2017-09-07 2023-07-01 Sage Therapeutics Inc Neuroactive steroids and their methods of use
TW202005653A (en) * 2018-06-12 2020-02-01 美商賽吉醫療公司 A 19-NOR C3,3-disubstituted C21-N-pyrazolyl steroid and methods of use thereof

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Publication number Publication date
AU2021312240A1 (en) 2023-02-02
US20230057130A1 (en) 2023-02-23
TW202220667A (en) 2022-06-01
AR123018A1 (en) 2022-10-26
US20230285417A1 (en) 2023-09-14
KR20230041049A (en) 2023-03-23
MX2023000835A (en) 2023-04-10
EP4181884A1 (en) 2023-05-24
JP2023537240A (en) 2023-08-31
IL299829A (en) 2023-03-01
CN116367827A (en) 2023-06-30
CL2023000176A1 (en) 2023-09-15
PE20231301A1 (en) 2023-08-24
CO2023001579A2 (en) 2023-03-07
WO2022020363A1 (en) 2022-01-27
WO2022020363A9 (en) 2022-03-10
CA3187178A1 (en) 2022-01-27
ECSP23012042A (en) 2023-03-31

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